科研之友
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摘要
The construction of a spiro-oxindole-based 2,5-dihydropyrrole scaffold with potential bioactivity has been established via an efficient three-component reaction of isatin, amino-ester and alkyne. This protocol represents the first 1,3-dipolar cycloaddition of electron-deficient alkynes with isatin-derived azomethine ylides, providing an easy access to spiro-oxindole-based 2,5-dihydropyrroles with structural diversity in high yields (up to 99%). In addition, the bioscreen of these new spiro-dihydropyrroles has led to the finding of sixteen compounds with promising cytotoxicity to MCF-7 cells.
